Pharm drugs by system Flashcards
Calcium-channel blockers
Block voltage-dependent L-type Ca channels, leads to decr. contractility
Dihydropyridines - act on vascular smooth muscle
- amlodipine, nifedipine, nicardipine
Non-DHP - act on cardiac muscle (aka Class IV)
- verapimil, diltiazem
Hydralazine
Vasodilates arterioles > veins, afterload reduction
Frequently co-administered with a B-blocker to prevent reflex tachycardia
Nitroprusside, fenoldopam
Meds in hypertensive emergency
Nitroprusside - short acting, incr. cGMP to incr. NO
Fenoldopam - D1 receptor agonist, systemic vasodilation to decr. BP
Nitroglycerin/nitrates
incr. NO to vasodilate vascular smooth muscle –> incr. cGMP
dilate veins»_space; arteries to decr. preload
treat reflex tachy with BBs
Statins
HMG-CoA reductase inhibs
stop conversion of HMG-CoA to mevalonate (competitive inhibitor)
SE: hepatotoxicity, myopathy
Cholecystyramine
Bile acid resins
prevent reabsorption of bile acids, liver uses cholesterol to make more
decr. absorption of fat-soluble drugs (incr. bleeding times)
Fibrates
upregulate lipoprotein lipase, increased TG clearance
also, activate PPAR-a to induce HDL synthesis
SE: myopathy, cholesterol gallstones
Classes of anti-arrhythmics
I: sodium channel blockers
II: B-blockers
III: potassium channel blockers
IV: calcium channel blockers
lidocaine, mexiletine
Class IB anti-arrhythmics
decr. AP duration - narrow the action potential graph
Best for post-MI
Pioglitazone/risoglitazone
Glitazones
Increase insulin sensitivity in peripheral tissue by binding PPAR-gamma transcription regulator
can cause weight gain from fluid retention
Exenatide
Linagliptin
GLP-1 analog
DPP-4 inhibitor
Both increase insulin and decrease glucagon
Demeclocycline
ADH antagonist (possibly competitive antag)
Used for SIADH
Omeprazole, lansoprazole, pantoprazole
Proton pump inhibitors
Irreversibly inhibit H/K ATPase in parietal cells
decr. serum Mg with chronic use
Ezetimibe
Prevent cholesterol absorption at brush border
Niacin
inhibits lipolysis
SE: red flushed face that decr. with NSAIDs
hyperglycemia, hyperuricemia
Digoxin
direct inhibition of Na/K ATPase
leads to increased contractility and decreased conduction through AV node
Orlistat
inhibits gastric/pancreatic lipase
used for weight loss
Milrinone
phosphodiesterase 3 inhibitor (normally metabolizes cAMP)
in cardiac muscle: incr. cAMP = incr. contractility
in vascular smooth muscle: incr. cAMP = vasodilation
Flutamide
Competitive antagonist for testosterone and DHT receptors in target cells
Used for prostate cancer (in combo with GnRH antags)
Flecainide, propafenone
Class IC anti-arrhythmics
Prolongs ERP in AV node- changes slope of graph, but no change in width
Use for SVTs
Contraindicated in ischemic heart disease
B-blockers
Class II anti-arrhythmics
Decr. cAMP –> decr. automaticity of pacemakers- decr. slope of funny current, wider graph
Use for AVT
SE: metop: dyslipidemia, propran: vasospasm in variant angina
Verapimil, diltiazem
Class IV anti-arrhythmics - L-type Ca channel blockers, non-DHP
slow funny current rise, prolonged repolarization
Aspirin
COX-1, COX-2 inhibitors (irreversible, lasts as long until new plts, 8-10 days)
Can cause gastric ulcers, tinnitus, Reye syndrome with viral infection
Aspart, lispro
Rapid-acting insulin
Cilostazol, dipyridamole
PDE III inhibitor
incr. cAMP –> decr. plt aggregation
Detemir, glargine
Long-acting insulin
Azathioprine/6-MP
purine analog –> block de novo purine synthesis
activated by HGPRT
metabolized by xanthine oxidase
Used to prevent organ rejection, RA, IBD, SLE
Glimepiride, glipizide, glyburide
Sulfonylureas
Close K channels in B cells to stimulate insulin release (so no good in Type 1 DM)
high risk of hypoglycemia
Methotrexate
Folate analog (DHF inhibitor)
Used for everything!
SE: myelosuppresion, hepatotoxicity, mucositis, pulmonary fibrosis
Methimazole
Blocks thyroid peroxidase
Contraindicated in pregnancy!
Conivaptan, tolvaptan
ADH antagonists, block action of ADH at V2 receptor
used in hyponatremia
Desmopressin
Used for central DI
Cinacalcet
Sensitizes CaSR in the parathyroid to serum Ca2+ therefore decreases PTH
Carmustine, lomustine
nitrosureas, alkylating (cross-links DNA)
requires bioactivation by liver
Used for brain tumors (accesses CNS)
Bismuth, sucralfate
Bind to stomach ulcer base, providing physical protection and allowing HCO3 secretion
Misoprostol
PGE1 analog –> incr. mucus barrier, decr. acid production
can cause diarrhea, is contraindicated in women of child-bearing potential
Octreotide
long-acting somatostatin analog
used for acute variceal bleeds, acromegaly, VIPoma, carcinoid tumors
AlOH, CaCO3, MgOH
Antacids
Can cause low K, affect other drugs by altering gastric pH
AlOH: constipation, low PO4
CaCO3: high Ca, rebound acid incr.
MgOH: diarrhea, hyporeflexia, cardiac arrest
Sulfasalazine
Combo of antibacterial and antiinflammatory
Uses for ulcerative colitis and colitis of Crohn’s
Ondansetron
5-HT3 antagonist, decr. vagal stimulation
Central-acting anti-emetic (good for chemo patients)
SE: headache, constipation, QT interval prolongation
Metoclopramide
D2 receptor antagonist –> incr. tone/contractility in gut
Used for diabetic gastroparesis
Incr. risk of tardive dyskinesia
Heparin
Antithrombin activator (decr. II and decr. X)
HIT: development of IgG against PF4, activating platelets –> thrombosis and thrombocytopenia (4 T’s)
Argatroban
direct thrombin inhibitors
Use in HIT sensitive patients
Warfarin
interfere w/ gamma-carboxylation of clotting factors
incr. PT (extrinsic pathway)
skin/tissue necrosis - small vessel microthromboses
Rivaroxaban
Directly inhibit factor Xa
No reversal agent available for bleeding
Alteplase (tPA), streptokinase
Thrombolytics
Incr. plasmin, incr. PT/PTT
Clopidogrel, ticlopidine
ADP receptor inhibitor (prevent expression of GpIIb/IIIa)
ticlopidine can cause neutropenia
Abciximab
GpIIb/IIIa inhibitor
prevent plt aggregation
made from Fab fragments
Cladribine
purine analog
used in hairy cell leukemia
Cytarabine
pyrimidine analog
Used for AML, lymphomas
5-FU
pyrimidine analog, covalently complexes folate (decr. dTMP, decr. DNA synthesis)
Used for colon cancer, pancreatic cancer
Bleomycin
antitumor antibiotic
free radical formation, creates breaks in DNA strand
can cause pulmonary fibrosis, skin hyperpigmentation
Actinomycin D
antitumor antibiotic
intercalates in DNA
used for childhood tumors
Doxorubibin, daunorubicin
antitumor antibiotic
generates free radicals and intercalates in DNA
Busulfan
alkylating (cross-links DNA)
used to ablate bone marrow before BMT
Cyclophosphamide
alkylating (cross-links DNA)
requires bioactivation by liver
can cause hemorrhagic cystitis
Paclitaxel
microtubule inhibitors (stabilized in M phase, no spindle breakdown)
Can cause alopecia, hypersensitivity
Vincristine, vinblastine
bind beta-tubulin and inhibit tubule formation (no spindle formation)
vincristine: periperal neuropathy
Cisplatin
cross-link DNA
high kidney and ear toxicity
prevent toxicity with amifostine (free radical scavenger) and chloride diuresis
Etoposide, teniposide
Inhibits topoisomerase II (dsDNA nicks), incr. DNA degradation
Irinotecan, topotecan
Inhibit topoisomerase I (single-strand nicks)
Hydoxyurea
Inhibit ribonucleotide reductase (decr. DNA synthesis)
good for melanoma, CML, sickle cell disease (incr. HbF)
Bevacizumab
VEGF monoclonal antibody
inhibits angiogenesis
Erlotinib
EGFR tyrosine kinase inhibitor
Used for non-small cell lung carcinoma
Trastuzumab
Herceptin, targets HER-2 overexpressing cells (breast/gastric cancer)
severe cardiotoxicity
Common chemotoxicities
Cisplatin/carboplatin - acoustic nerve damage, nephrotoxicity Vincristine - peripheral neuropathy Bleomycin, busulfan - pulmonary fibrosis Trastuzumab - cardiotoxicity Doxorubicin - cardiotoxicity Cyclophosphamide - hemorrhagic cystitis 5-FU, 6-MP, MTX - myelosuppression
Albuterol
b2 > b1 (relaxes bronchial smooth muscle)
asthma
Dobutamine
B1 > B2
heart failure (incr. inotropy)
Dopamine
D1, D2
at intermediate doses, stimulates beta, stimulates inotropy, chronotropy
at high doses, stimulates alpha, vasoconstriction = decr. CO
Epinephrine
Beta > alpha (B1: renin –> increased vascular tone, B2: relaxes constricted airways)decreased mast cell degranulation, increased heart activity)
treat anaphylaxis, asthma, open-angle glaucoma
Isoproterenol
B1/B2
evaluation of tachyarrhythmias (positive chronotropy, inotropy)
Norepinephrine
alpha 1 > alpha 2 > beta 1
treats hypotension (alpha 1 causes vasoconstriction, used in shock)
Phenylephrine
alpha 1 > alpha 2
Hypotension (vasoconstrictor), ocular procedures (mydriatic), rhinitis (decongestant)
Clonidine
Alpha 2
central acting, leads to vasodilation
Ranitidine, cemetidine, famotidine
reversible H2 receptor blocker, decr. acid by parietal cells
Cemetidine = cytochrome p450 inhibitor, anti-androgen, cross BBB and placenta, incr. serum Cr.
Decr. gastric acid production
Acetaminophen
CNS Cox reversible inhibitor
not anti-inflammatory
tox: depletes glutathione, requires NAC to regenerate
Aspirin
COX 1/2 irreversible inhibitor via acetylation, decr. TxA2 and PGs
dose: low (anti-platelet), medium (antipyretic/analgesic), high (anti-inflammatory)
incr. bleeding time, no effect on PT/PTT
can cause gastric ulcers and tinnitus
Celecoxib
Reversibly inhibit COX-2
no effect on GI lining or platelet function
NSAIDs
reversibly inhibit COX1/2
note: can cause renal ischemia (prevent vasodilatory effects of prostaglandins)
Alendronate, -dronates
bisphosphonate, inhibit osteoclast activity
can cause erosive esophagitis
Teriparatide
PTH analog, increase osteoblast activity
(though chronic exposure to PTH bone resorption, intermittent will cause bone building)
causes transient hypercalcemia
Allopurinol
inhibit xanthise oxidase (decr. uric acid production)
chronic gout drug
note: incr. axathioprine/6-MP (usually metabolized by XO)
Probenecid
decr. reabsorption of uric acid in proximal convoluted tubule (uricosuric agent)
chronic gout drug
can cause uric acid calculi (kidney stones)
Colchicine
bind and stabilize tubulin, impair neutrophil chemotaxis and degranulation
can be used acutely and prophylactically in gout treatment
Etanercept
fusion protein, TNF decoy receptor
used in rheumatoid arthritis, psoriasis, ankylosing spondylitis
incr. risk of infection, notably TB reactivation
Infliximab, adalimumab
anit-TNF monoclonal antibody
IBS, RA, ank spondy, psoriasis
incr. risk of infection, notably TB reactivation
Butorphanol
kappa-opioid receptor agonist and mu partial agonist
Tramadol
weak opioid agonist, also inhibits 5-HT and NE reuptake
also decreases seizure threshold
Ethosuximide
block T-type Ca channels in thalamus
absence seizures
watch for urticaria, SJS (prodrome then rash then necrosis/sloughing)
Phenytoin
Na channel inactivation
use for all seizures
Lots of side effects! SLE-like syndrome, SJS, gingival hyperplasia
Phenobarbital
incr. duration of Cl channel opening –> incr. GABA
use as sedative
induces cytochrome p450
Benzodiazepines
incr. frequency of Cl channel opening –> incr. GABA
less risk of resp. depression than barbs
treat overdose with flumazenil (competitive antagonist)
Zolpidem, zaleplon, eszopiclone
BZ1 subtype of GABA receptor
used for insomnia
short duration, decr. aftereffects
Ketamine
Block NMDA receptors
cardiovascular stimulants (dissociative anesthetics)
increase cerebral blood flow
Propofol
potentiates GABA-A
rapid induction
Succinylcholine
strong ACh receptor agonist, sustained depol and prevents muscle contraction
Phase 1 block: block potentiated by AChEis
Phase 2 block: desensitized Ach receptors, allows for cholinesterase inhibitors to be used an antidote
Vecuronium, rocuronium
Competitive ACh antagonist, use for patients with arrhythmias/electrolyte disturbances
reverse blockade with neostigmine+atropine, edrophonium
Baclofen
GABA-B agonist at spinal level
skeletal muscle relaxant (use for muscle spasms)
Cyclobenzaprine
Centrally acting skeletal muscle relaxant
Bromocriptine, ripinorole
Dopamine agonists
used in parkinson’s
Amantadine
incr. dopamine release and decr. dopamine reuptake
use for Parkinson’s
(also antiviral against influenza A/rubella)
Selegiline
MAO-inhibitor
blocks conversion of dopamine to 3-MT, incr. DA levels
Memantine
NMDA receptor antagonist
Alzheimer’s
Donepezil
AChE inhibitor
Alzheimer’s
Sumitriptan
5-HT 1B/1D
inhibit trigeminal nerve activation, induce vasoconstriction
acute migraine, cluster headaches
can cause coronary vasospasm
Mannitol
Osmotic diuretic (increases tubular fluid osmolarity) Also decreases intracranial and intraocular pressure
Acetazolomide
carbonic anhydrase inhibitor
causes hyperchloremic metabolic acidosis
urinary alkalinization
Furosemide
Loop diuretic - inhibit Na/K/2Cl of thick ascending loop
Abolish medullary hypertonicity, preventing concentration of urine
Stimulate PGE release, vasodilates afferent arteriole
increased Ca secretion
toxicity: ototoxicity, hypoK, dehydration, allergy (to sulfa), Nephritis, Gout
if allergy, give ethacrynic acid
Hydrochlorothiazide
inhibit NaCl reabsorption in early DCT
decreases Ca excretion
tox: hyperGLUC (glycemia, lipidemia, uricemia, calcemia)
Amiloride
K sparing diuretic, block ENaC in cortical collecting tubule
can cause hyperkalemia (peaked T waves)
Enalapril, captopril
Inhibit ACE conversion to AT-II, decr. GFR (prevents constriction of efferent arteriole)
incr. renin, prevents inactivation of bradykinin (leads to vasodilation and cough)
tox: cough, angioedema, teratogen, incr. Cr, hyperK, hypotension (avoid in bilateral renal artery stenosis)
Losartan, candesartan
block binding of AT II to AT-1 receptor
no effect on bradykinin
Aliskiren
Direct renin inhibitor
contraindicated in DM pts taking ACEis or ARBs
Leuprolide
GnRH analog; agonist when pulsatile, antagonist when used continuously
pulsatile use: infertility
continuous use: prostate cancer, uterine fibroids, precocious puberty
Clomiphene
in hypothalamus, estrogen receptor antagonist. leads to incr. LH, FSH secretion from ant. pit.
used to stimulate ovulation (in PCOS)
Anastrozole, exemestane
aromatase inhibitors
used in post-menopausal women with ER-positive breast cancer
Mifepristone
competitive inhibitor at progesterone receptors
used to terminate pregnancy
Terbutaline, ritodrine
B2-agonists that relax the uterus
Danazol
partial androgen agonist
used for endometriosis, hereditary angioedema
Testosterone
Agonists at androgen receptors
Finasteride
5a-reductase inhibitor (prevent conversion of testosterone to DHT)
used in BPH and baldness
Flutamide
Competitive inhibitor at androgen receptor
used for prostate cancer
Ketoconazole
inhibit steroid synthesis (inhibits 17,20 desmolase)
treats PCOS to reduce androgen symptoms
can cause gynecomastia and amenorrhea
Tamsulosin
alpha-1 antagonist (inhibit smooth muscle contraction)
used to treat BPH, selective for prostate alpha-1 receptors vs. vascular alpha-1 receptors
Diphenhydramine, chlorpheniramine
H1 reversible receptor blocker (1st gen)
tox: sedation, antimuscarinic, anti- alpha adrenergic
Loratidine, fexofenadine
H1 reversible receptor blocker (2nd gen)
Far less sedating than 1st generation, decr. entry into CNS
Guaifenesin
expectorant, thins respiratory secretions
Dextramethorphan
NMDA glutamate receptor antagonist
codeine analog, mild opioid effect when used in excess
Antitussive
may cause serotonin syndrome
Pseudoephedrine, phenylephrine
alpha agonist
nasal decongestant
Bosentan
Endothelin-1 antagonist
used to treat pulmonary hypertension
Epoprostenol
PGI2 analog
direct vasodilatory effect on pulmonary and systemic arterial vascular beds
used to treat pulmonary hypertension
Ipratropium
muscarinic antagonist
Prevents bronchoconstriction
used for asthma and COPD
Theophylline
phosphodiesterase inhibitor, incr. cAMP (decr. cAMP hydrolysis)
narrow therapeutic index (cardio/neurotoxic)
blocks adenosine
Tacrolimus
Antitumor antibiotic
Inhibits calcineurin-mediated transcription of IL-2 (binds FK506 binding protein)
Cyclosporine
Binds cyclophillin
Inhibits calcineurin-mediated transcription of IL-2
Acyclovir, valcyclovir
Guanosine analog, phosphorylated in infected cells
Used against HSV, VZV (have the required phosphorylase)
Ganciclovir
Guanosine analog, phosphorylated only in CMV cells
Foscarnet
Viral RNA/DNA polymerase inhibitor and HIV reverse transcript inhibitor
Pyrophosphate analog
Causes hypocalcemia and hypomagenesemia
Cidofovir
inhibits viral DNA polymerase, NO phosphorylation required!
2nd line for CMV and HSV
